Details for Patent: 8,481,078

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Summary for Patent: 8,481,078

Title:	Solid dosage form comprising a fibrate
Abstract:	The invention provides stable, solid dosage forms and pharmaceutical compositions in particulate form comprising a fibrate, for example fenofibrate, dissolved in an non-aqueous vehicle in order to ensure improved bioavailability of the active ingredient upon oral administration relative to known fibrate formulations.
Inventor(s):	Per Holm, Tomas Norling
Assignee:	Veloxis Pharmaceuticals Inc
Application Number:	US13/315,030
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;

Scope and Claim Strength of US Patent 8,481,078 (Fenofibrate Immediate-Release Tablets Using Meltable Vehicles, PEG/Poloxamer, and Sprayed Particles)

US 8,481,078 is a composition-and-process patent that centers on immediate-release (IR) fenofibrate embedded in meltable “vehicles” at specified melting-point ranges, particle size distributions, and fenofibrate loading. The estate is narrow in identity of the active (fenofibrate only) and dosage form (tablets/solid dosage made from sprayed particles on carriers), but broad across polymer families that can function as the melting vehicle (PEGs, poloxamers, EOs, PEO-stearates, HPMC/MC, PVPA/PVP systems, etc.). Enforcement leverage is strongest for IR fenofibrate solid dosage where (i) the fenofibrate is dispersed in a vehicle that melts in the claimed window (about 30–100°C, with preferred subranges), (ii) sprayed onto/into solid-carrier particles of specified dgw, and (iii) the product meets a defined in vitro release criterion (≥75% in ~45 min in specific paddle conditions for dependent claim 14).

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What is US 8,481,078 about and what invention does it claim?

Featured snippet answer: US 8,481,078 claims IR fenofibrate tablets/solid dosage forms made from sprayed particles where fenofibrate is in a meltable polymer “vehicle” (melting point ~30–100°C), with defined particle size (dgw ~20–2000 μm) and fenofibrate loading (~10–70 wt%), including embodiments using PEG or poloxamer (e.g., Poloxamer 188/407) and optional hydrogenated castor oil.

What the claims are structurally doing

Across independent claims (1, 15, 19, 22), the patent repeatedly uses the same claim “stack”:

1. Drug identity: fenofibrate only.
2. Form factor: tablet or solid dosage form made via sprayed particles on a solid carrier; tablets can be compressed.
3. Particle architecture: particles comprising:
   • solid carrier plus
   • fenofibrate in a vehicle (vehicle has a defined melting point range).
4. Vehicle physical property constraint: melting point about 30°C to 100°C (or narrowed ranges such as 40–75°C and 40–70°C).
5. Particle size constraint: dgw about 20 μm to 2000 μm (with narrower dependent ranges such as 100–400 μm).
6. Fenofibrate loading constraint: about 10% to 70% by weight fenofibrate based on total fenofibrate + vehicle (in some embodiments 10–35 wt% and specific ratios for poloxamer).
7. Performance constraint: “immediate release,” plus a specific dissolution test in dependent claim 14.

Immediate-release definition in the patent

Dependent claim 14 is the clearest “objective” performance gate:

• At least 75% fenofibrate released within ~45 minutes
• Using Ph. Eur. paddle dissolution test
• Water with 0.75% sodium lauryl sulfate
• 50 rpm, 37°C

That dependent claim is important for freedom-to-operate (FTO) because it converts “immediate release” from a marketing/functional label into a measurable criterion.

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What are the key independent claims and their scope (US 8,481,078 claims 1, 15, 19, 22)?

Claim 1 (tablet with sprayed-meltable vehicle particles)

Core scope: A tablet comprising particles with:

• solid carrier + fenofibrate in a vehicle
• vehicle melting point 30–100°C
• particle dgw 20–2000 μm
• fenofibrate 10–70 wt% (fenofibrate/vehicle basis)
• tablet provides immediate release

Dependent narrowing in claim set:

• dgw 100–400 μm (claim 2)
• vehicle melting point 40–75°C (claim 3) and 40–70°C (claim 4)
• vehicle hydrophilic (claim 5)
• explicit polymer lists for vehicle composition (claims 6–11)
• explicit Poloxamer embodiments and fenofibrate:poloxamer ratio (claims 9–12)
• compressed tablet (claim 13)
• dissolution performance (claim 14)

Practical reading: To infringe claim 1, an accused product must satisfy all structural constraints (melting point window, dgw, loading) and be an IR fenofibrate tablet made from particles in that architecture.

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Claim 15 (solid dosage form with sprayed fenofibrate on carrier)

Core scope: Solid dosage form comprises particles formed by:

• solid carrier sprayed with fenofibrate in vehicle
• vehicle melting point 30–100°C
• particles dgw 20–2000 μm
• fenofibrate 10–70 wt%
• IR fenofibrate

Practical reading: Claim 15 is the composition/particle product claim for the “sprayed on carrier” route, without limiting to a compressed tablet.

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Claim 19 (method of preparation by spraying onto a carrier at < melt point)

Core scope: A process:

• (a) spraying a mixture of fenofibrate + liquid vehicle onto a solid carrier, where carrier is at temperature below the melting point of the vehicle
• vehicle melting point 30–100°C
• (b) forming a solid dosage form from the particles
• same dgw and fenofibrate loading constraints
• IR performance

Practical reading: Claim 19 adds a process condition (carrier temperature below vehicle melting point). This can matter for design-around: changing process temperatures may avoid literal infringement, though doctrine of equivalents can be argued depending on claim construction.

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Claim 22 (tablet with poloxamer and specific fenofibrate:poloxamer loading and preparation steps)

Core scope:

• tablet comprises fenofibrate in a vehicle comprising poloxamer
• fenofibrate 10–35 wt%
• prepared by spraying mixture of fenofibrate + poloxamer onto solid carrier, then forming tablet
• IR fenofibrate

Practical reading: Claim 22 is a more specific embodiment of claim 1, anchored to poloxamer as the vehicle and a narrower loading range.

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What vehicle compositions are covered (PEG, poloxamers, PVP/PVA, HPMC, cyclodextrins, castor derivatives)?

Claim 1 uses “vehicle having a melting point” plus dependent claims that list example polymers and excipients. The legal significance is that the lists create multiple embodiments that can be separately targeted for infringement.

Claim 6 vehicle examples (broad polymer family list)

Vehicle may comprise one or more of:

• polyethylene glycol
• poloxamers
• polyoxyethylene stearates
• poly-epsilon-caprolactone
• polyvinylpyrrolidone (PVP)
• PVP-polyvinylacetate copolymer
• polymethacrylic polymers
• polyvinyl alcohol (PVA)
• hydroxypropyl cellulose
• hydroxypropyl methyl cellulose (HPMC)
• methyl cellulose
• poly(ethylene oxide)

Claim 7 vehicle examples (expanded list)

Vehicle may comprise one or more of:

• polyoxyethylene oxide and related polymeric systems
• cyclodextrins, galactomannans, alginates, carragenates, xanthan gums
• carrageenates (spelling in claim)
• plus additional cellulose and acrylic/methacrylic polymer classes
• includes myristyl alcohol
• includes sodium carboxymethylcellulose, hydroxyethyl cellulose, pectins
• includes mixtures

Claim 8 vehicle examples (specific meltable EO/PO systems)

Vehicle comprises one or more of:

• polyoxyethylene oxide
• polyoxyethylene stearate
• poly-epsilon-caprolactone
• mixtures

Claims 9–12 poloxamer-specific coverage

Vehicle comprises poloxamer; dependent claims specify:

• poloxamer 188 or poloxamer 407
• fenofibrate:poloxamer weight ratio about 3:1 to 1:20 (claim 12)

Claims 24–26 PEG, and claims 27–29 hydrogenated castor oil

Dependent claims explicitly include:

• vehicle comprises polyethylene glycol
• vehicle comprises hydrogenated castor oil

Enforcement implication: An accused IR fenofibrate tablet that uses poloxamer, PEG, or hydrogenated castor oil can be attacked with both the general meltable-vehicle constraints and those dependent identity constraints, depending on the product’s exact formulation.

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What particle size (dgw) and fenofibrate loading limits matter most for claim coverage?

Particle size distribution: dgw

• Independent baseline: dgw ~20–2000 μm (claims 1, 15, 19)
• Narrow dependent: dgw 100–400 μm (claims 2 and 16; and mirrored in process context for claim 20)

Risk lens: If a generic or reformulation targets substantially smaller or larger dgw outside the window, it can reduce literal infringement exposure. If the accused product reports different PSD metrics, a claim-construction fight may arise around equivalence of “dgw” measurement and comparable distributions.

Fenofibrate loading

• Baseline: 10–70 wt% fenofibrate (claims 1, 15, 19)
• Poloxamer embodiment: 10–35 wt% fenofibrate (claim 22)

Risk lens: Many commercial formulations may use lower effective drug loads per unit mass with excipients and release modifiers. The claim’s loading basis is “based upon 100% total weight of the fenofibrate and vehicle.” That is a narrower denominator than “tablet weight,” which can materially change infringement analysis.

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When does US 8,481,078 expire and when do exclusivity barriers turn off?

No filing date, priority date, or term adjustments were provided in the prompt. Without those dates, it is not possible to state an accurate expiration date or exclusivity timeline.

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What patent landscape surround US 8,481,078 likely includes: immediate-release fenofibrate formulation and particle-spray technologies?

Given only the claim text, the scope can be mapped to adjacent innovation lanes that commonly co-exist in fenofibrate formulation portfolios:

• meltable polymer vehicles with defined melting-point windows
• sprayed dispersions on inert carriers to control PSD (dgw)
• PVP/PVA/HPMC and EO/EO-stearate melt-capable binders
• poloxamer-based solid dispersions/IR release systems
• conversion of sprayed particles to compressed tablets
• dissolution performance aligned to pharmacopeia paddle methods

However, without the patent family details (priority/family members), assignee, and citation list, a comprehensive US competitor landscape (including other patent numbers, listed assignees, or Paragraph IV filings) cannot be constructed from the provided inputs.

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How strong is the claim set: what elements create the highest “infringement friction”?

Highest-friction elements (typically hardest to prove or easiest to design around)

1. Vehicle melting point window (30–100°C)

   • Many formulations use amorphous dispersions or surfactants without a melt-defined polymer vehicle. If the “vehicle” in an accused product is not characterized to fall inside the claimed melting point range, literal infringement weakens.

2. Particle size “dgw” (20–2000 μm)

   • Particle engineering and characterization can be a major differentiator. Even if IR release is achieved, PSD may fall outside the dgw window.

3. Fenofibrate loading basis (10–70 wt% based on fenofibrate + vehicle)

   • Formulas often include multiple excipients outside “vehicle.” If the accused product’s “vehicle” does not match the claim’s fenofibrate+vehicle basis, infringement analysis changes.

4. Spraying method temperature condition (claim 19)

   • Claim 19 requires the solid carrier be at a temperature below the melting point of the vehicle during spraying. Alternative coating/spraying thermal histories may avoid literal process infringement.

Medium-friction elements

• polymer identity lists (PEG, poloxamer, PVP, HPMC, etc.)
• hydrophilicity (claim 5) can be lab-defined but is less deterministic than melting point and PSD.

Lower-friction elements

• “immediate release” is functional, but claim 14 supplies a measurable dissolution target that can become high-friction if tested conditions match.

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What generic entry risks exist for fenofibrate IR tablets under US 8,481,078?

Primary risk scenario: A generic or authorized generic that copies the same particle-spray architecture using a meltable vehicle with comparable melting point, PSD, and loading, and achieves the same pharmacopeial IR dissolution performance.

Design-around levers (based on claim text):

• Shift vehicle chemistry or formulation so the “vehicle” does not have a melting point within 30–100°C (or preferred 40–75°C/40–70°C ranges).
• Use a carrier/vehicle system yielding dgw outside 20–2000 μm, including targeting outside 100–400 μm.
• Adjust fenofibrate:vehicle ratio so the fenofibrate-by-vehicle loading moves outside 10–70 wt% or outside 10–35 wt% in poloxamer embodiments.
• Avoid the spraying process-temperature condition required by claim 19 (if aiming to reduce process infringement).
• For poloxamer-based products, alter the ratio outside 3:1 to 1:20 and/or substitute a non-poloxamer vehicle.

These are claim-text grounded tactics; actual risk depends on product characterization, labeling, and litigation claim construction.

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How does US 8,481,078 compare with other common fenofibrate formulation patent themes?

From the claim structure alone, US 8,481,078 sits in the overlap of:

• solid dispersion/solubilization (meltable vehicle carrying fenofibrate)
• spray-on carrier particle engineering (dgw targeting)
• IR release performance (pharmacopeia paddle dissolution metric)

In contrast, patents that focus only on:

• micronization without a defined meltable vehicle,
• capsule shells or coating layers unrelated to meltable vehicles,
• prodrug or salt forms,
• or alternative release profiles (sustained/enteric release) would generally not meet the melt-point + dgw + loading + spraying-defined architecture at the claim level.

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What FDA regulatory status and Orange Book status apply to US 8,481,078?

The prompt does not provide:

• the specific marketed fenofibrate product (brand name/NDA),
• the Orange Book listing number(s),
• or any FDA regulatory milestones tied to this patent.

Without that mapping, the FDA/Orange Book status cannot be stated.

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Key Takeaways

• US 8,481,078 claims IR fenofibrate tablets/solid dosage forms built from sprayed particles using a meltable vehicle with melting point 30–100°C, particle dgw 20–2000 μm, and fenofibrate loading 10–70 wt% (fenofibrate+vehicle basis).
• Dependent claims add strong attack surface via:
  • vehicle melting point narrowing (40–75°C; 40–70°C),
  • particle size narrowing (100–400 μm),
  • explicit vehicle polymer lists including PEG, poloxamers (188/407), PVP/PVA/HPMC/MC, EO-stearates, cyclodextrins, alginates/xanthan/carrageenates, and hydrogenated castor oil,
  • specific poloxamer fenofibrate:poloxamer weight ratios (3:1 to 1:20),
  • and a concrete dissolution performance test (≥75% release in ~45 min under Ph. Eur. paddle with 0.75% SLS at 37°C).
• The highest infringement-friction points are likely vehicle melting point, dgw, and fenofibrate-by-vehicle loading, with claim 19’s process temperature as an additional design-around lever.
• Expiration timing, Orange Book status, and any Paragraph IV or litigation posture cannot be concluded from the provided information.

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FAQs

1. What product characteristics most directly determine infringement risk for US 8,481,078?
   Vehicle melting point (30–100°C), particle dgw (20–2000 μm), fenofibrate loading on a fenofibrate+vehicle basis (10–70 wt%), and IR release performance.

2. Does US 8,481,078 require poloxamer to infringe?
   No. Poloxamer is a dependent embodiment (claims 9–12) within a broader meltable-vehicle scope in claim 1.

3. How does claim 14 change “immediate release” into an evidentiary test?
   It ties IR to a measurable dissolution outcome: at least 75% released within ~45 minutes using a defined Ph. Eur. paddle method and dissolution medium/conditions.

4. Can a reformulation avoid claim 19 by changing process temperatures?
   Claim 19 requires the solid carrier be at a temperature below the vehicle’s melting point during spraying; altering that condition is a direct literal-design lever.

5. If a product uses PEG, is it automatically within the patent?
   PEG can be within the listed vehicle examples, but infringement still requires the claimed melting point window, dgw range, fenofibrate loading, and IR performance tied to the claimed architecture.

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References (APA)

1. US Patent 8,481,078 (claims as provided in prompt).

Drugs Protected by US Patent 8,481,078

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 8,481,078

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2004279661
Australia	2009201881
Brazil	PI0415121
Canada	2540984
Canada	2541382